α-Glucosyl hesperidin suppressed the exacerbation of 5-fluorouracil-induced oral mucositis in the hamster cheek pouch

• Hsp-G indicated antioxidant activity towards superoxide and hydroxyl radical.
• Hsp-G administration did not affect the body weight change of the hamster.
• Pre-treatment with Hsp-G inhibited exacerbation of oral stomatitis and an increase of TBARS levels.
• Hsp-G did not affect the anti-tumour activity of 5-FU on HSC-3 cells.

Hesperidin (Hsp), the so-called vitamin P, is an abundant flavonoid in citrus fruits and exerts many biological functions, including antioxidative, anti-inflammatory and anticarcinogenic activities. However, Hsp is not adequately soluble in aqueous solutions and not absorbed well through the intestinal tract. α-glucosyl hesperidin (Hsp-G) is a derivative of Hsp with enhanced water-solubility, while it retains the natural biological functions of Hsp. In this study, the biological functions of Hsp-G on oral stomatitis were examined. Hsp-G exhibited scavenging activity towards hydroxyl radical and superoxide anion radical. Oral stomatitis areas were significantly smaller in hamsters administered Hsp-G than in the non-administered group. Increases in thiobarbituric acid reactive substances, expressed as malondialdehyde equivalents, levels were significantly inhibited by the pre-treatment with Hsp-G prior to the administration of 5-fluorouracil. Hsp-G had no effect on anti-tumour activity in human oral squamous carcinoma cells. Therefore, Hsp-G may serve as a functional food ingredient to ameliorate the symptoms of oral stomatitis.